Drug intelligence / Profile preview

thiamet G

Development stage
Preclinical
Lead developer
Simon Fraser University
Modality
Small Molecules
Administration
Oral
01

Overview

Thiamet G is a potent, highly selective, and cell-permeable small molecule inhibitor of O-GlcNAcase (OGA), the enzyme responsible for removing O-linked N-acetylglucosamine (O-GlcNAc) modifications from nucleocytoplasmic proteins. By inhibiting OGA, Thiamet G increases the global levels of O-GlcNAcylation on various proteins, which can modulate their stability, localization, and activity. It is widely used as a pharmacological tool in research to study the role of O-GlcNAc signaling in diverse biological processes, including neurodegeneration (e.g., Alzheimer's disease), metabolism, and reproductive biology. In the context of ovarian tissue research, it has been used to demonstrate that hyper-O-GlcNAcylation can destabilize transcription factors like FOXL2, leading to reduced estrogen synthesis.

Other names
Thiamet-G
02

Targets

OGA (Protein O-GlcNAcase)

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